Primary Bioactive Components Research Articles

Investigating the Therapeutic Mechanisms of Total Saikosaponins in Alzheimer’s Disease: A Metabolomic and Proteomic Approach

Alzheimer’s disease (AD) is the leading cause of dementia among the elderly, yet effective treatments remain elusive. Total saikosaponins (TSS), the primary bioactive components in Bupleurum chinense, have shown promising therapeutic effects against AD in previous studies. Methods: To delve deeper into the mechanisms underlying the therapeutic role of TSS in AD, we investigated its neuroprotective effects and associated molecular mechanisms in APP/PS1 mice. Further, we employed metabolomic and proteomic analyses, with a focus on the potential protein-level changes induced by TSS, particularly those related to metabolite accumulation in the brain. Results: Our results showed that lysophosphatidylcholine, adenosine, and sphingomyelin in plasma might serve as potential biomarkers. Compared to the control group, AD mice exhibited significantly increased expression of proteins related to neuroinflammatory pathways, whereas proteins involved in cAMP signaling, cGMP-PKG signaling, and synaptic plasticity pathways were significantly downregulated. Notably, these signaling pathways were partially reversed in APP/PS1 mice following TSS administration. Behavioral tests demonstrated that TSS effectively improved the learning and memory functions of mice. Conclusions: Our findings suggest that TSS ameliorate cognitive decline through regulating neuroinflammatory pathways, cAMP and cGMP signaling, and synaptic plasticity pathways, providing insights into its therapeutic potential in AD.

Two-Component Hydrogels Built from Chinese Herbal Medicine-Derived Glycyrrhizic Acid and Puerarin: Assembly Mechanism, Self-Healing Properties, and Selective Antibacterial Activity.

Chinese herbal medicine has offered a great treasure for discovering intrinsically bioactive low molecular weight gelators (LMWGs). Herein, the two-component hydrogels comprising glycyrrhizic acid (GA) and puerarin (PUE), the primary bioactive components, respectively, from herbs Glycyrrhiza uralensis Fisch and Pueraria lobata are successfully prepared. Combined spectroscopic characterizations reveal that hydrogen bonds are formed between GA and PUE molecules, which further drives the growth of nanofiber assemblies into gel networks. Importantly, micromorphological observation by scanning electron microscopy (SEM), synchrotron small-angle X-ray scattering (SAXS), and molecular dynamic simulation suggest that a coassembly pathway is involved in the gelling process. Such two-component hydrogels exhibit good injectable, self-healing, and adhesive properties. Interestingly, the mixed GA-PUE hydrogels demonstrate a more efficient and selective antibacterial activity toward S. aureus instead of E. coli, and a PUE ratio-dependent antibacterial activity toward S. aureus is also observed. Our work highlights that CHM-derived LMWGs can provide a scaffold for developing multicomponent hydrogels, which may afford novel and distinct properties compared with their individual ones. It is assumed that more multicomponent supramolecular hydrogels derived from CHM would appear to better address the challenges, particularly in the biomedical field.

Investigation of Anti-Apoptotic Effects and Mechanisms of Astragaloside IV in a Rat Model of Cerebral Ischemia-Reperfusion Injury.

Ischemic stroke is a prevalent and life-threatening cerebrovascular disease that is challenging to treat and associated with a poor prognosis. Astragaloside IV (AS-IV), a primary bioactive component of Astragali radix, has demonstrated neuroprotective benefits in previous studies. This study aimed to explore the mechanisms through which AS-IV may treat cerebral ischemia-reperfusion injury (CIRI). Network pharmacology was employed to identify key targets and pathways of AS-IV in CIRI therapy, combined with molecular docking to predict binding affinity. Male Sprague-Dawley rats were randomly assigned to sham, MCAO/R, AS-IV, SP600125 (JNK inhibitor), AS-IV + SP600125, and 3-n-Butylphthalide (NBP) groups. Neurobehavioral deficits were assessed, and brain tissue damage was visualized through 2,3,5-triphenyltetrazolium chloride, H&E, and TUNEL staining. Immunohistochemistry was employed to detect CytC- and caspase-3-positive cells, while Western blotting, qPCR, and ELISAs were used to analyze apoptosis-related markers. A total of 48 key targets of AS-IV predicted to be involved in the treatment of CIRI were identified, enriched in 136 pathways. AS-IV was effectively bound to the top five targets from 48 targets, and those associated with the c-Jun N-terminal kinase (JNK)/Bid pathway, with binding energy values below -5.0 kJ·mol-1. JNK inhibition reduced infarcted brain areas, improved neurological function, reduced pathological brain tissue damage, and inhibited apoptosis, with AS-IV achieving similar neuroprotective effects. Both AS-IV and SP600125 reduced p-JNK, Bid, CytC, Apaf-1, caspase-3, and cleaved caspase-3 levels in rats while decreasing CytC, caspase-3, and caspase-9 levels in serum. AS-IV may suppress apoptosis partly through the modulation of JNK/Bid signaling, exerting neuroprotective effects. These findings support the potential development of AS-IV-based therapies for stroke treatment.

Polyphenols and Microbiota Modulation: Insights from Swine and Other Animal Models for Human Therapeutic Strategies.

High consumption of ultra-processed foods, rich in sugar and unhealthy fats, has been linked to the onset of numerous chronic diseases. Consequently, there has been a growing shift towards a fiber-rich diet, abundant in fruits, vegetables, seeds, and nuts, to enhance longevity and quality of life. The primary bioactive components in these plant-based foods are polyphenols, which exert significant effects on modulating the gastrointestinal microbiota through their antioxidant and anti-inflammatory activities. This modulation has preventive effects on neurodegenerative, metabolic, and cardiovascular diseases, and even cancer. The antimicrobial properties of polyphenols against pathogenic bacteria have significantly reduced the need for antibiotics, thereby lowering the risk of antibiotic resistance. This paper advances the field by offering novel insights into the beneficial effects of polyphenols, both directly through the metabolites produced during digestion and indirectly through changes in the host's gastrointestinal microbiota, uniquely emphasizing swine as a model highly relevant to human health, a topic that, to our knowledge, has not been thoroughly explored in previous reviews. This review also addresses aspects related to both other animal models (mice, rabbits, and rats), and humans, providing guidelines for future research into the benefits of polyphenol consumption. By linking agricultural and biomedical perspectives, it proposes strategies for utilizing these bioactive compounds as therapeutic agents in both veterinary and human health sciences.

Enhancing cancer therapy: advanced nanovehicle delivery systems for oridonin.

Oridonin (ORI), an ent-kaurane diterpenoid derived from Rabdosia rubescens (Hemsl.) H.Hara, serves as the primary bioactive component of this plant. It demonstrates a broad spectrum of therapeutic activities, including moderate to potent anticancer properties, alongside anti-inflammatory, antibacterial, antifibrotic, immunomodulatory, and neuromodulatory effects, thus influencing diverse biological processes. However, its clinical potential is significantly constrained by poor aqueous solubility and limited bioavailability. In alignment with the approach of developing drug candidates from natural compounds, various strategies, such as structural modification and nanocarrier systems, have been employed to address these challenges. This review provides an overview of ORI-based nano-delivery systems, emphasizing their potential to improve the clinical applicability of oridonin in oncology. Although some progress has been made in advancing ORI nano-delivery research, it remains insufficient for clinical implementation, necessitating further investigation.

The Protective Role of Baicalin in the Regulation of NLRP3 Inflammasome in Different Diseases.

The NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome consists of pro-caspase-1, NLRP3 and apoptosis-related speckle-like protein (ASC). It can detect multiple microorganisms, endogenous danger signals and environmental stimulus including adenosine triphosphate (ATP), urate, cholesterol crystals, and so on, thereby forming activated NLRP3 inflammasome. During the course of the activation of NLRP3 inflammasome, pro-caspase-1 is transformed into activated caspase-1 that results in the maturation and secretion of interleukin-1beta (IL-1β) and IL-18. The dysfunction of NLRP3 inflammasome participates in multiple diseases such as liver diseases, renal diseases, nervous system diseases and diabetes. Baicalin is the primary bioactive component of Scutellaria baicalensis, which has been used since ancient times. Baicalin has many types of biological functions, such as anti-bacterial, anti-tumor and antioxidant. More and more evidence suggests that baicalin regulation of NLRP3 inflammasome is involved in different diseases. However, the mechanism is still elusive. Here, we reviewed the progress of baicalin regulation of NLRP3 inflammasome in many kinds of diseases to lay a foundation for future researches.

RP-HPLC Method for Simultaneous Quantification of Withanolides in <i>Withania somnifera</i>

Background: Withanolides are the primary bioactive components of Withania somnifera (L.) Dunal. Among them, withanolide A, and 12-deoxy-withastramonolide are the herb’s most physiologically active ingredients. The steroidal lactones are isomers, which makes them difficult to separate. Aim: In the current research, a simple, precise, accurate, and decent RP-HPLC method has been developed, optimised and validated for simultaneous quantification and separation. Methods: Resolution was conducted on Gemini, Phenominex C18 (250mm X 4.6mm, 5 μ) column at 40oC utilising binary mobile phases of acetonitrile and ammonium acetate (10 mM) in gradient mode with 1.0 mL/min flow rate and observed at 230 nm. The total run time was twenty-five minutes. The procedure complied with ICH guidelines, covering the limit of detection, specificity, linearity, quantification, precision, accuracy, and robustness. Results: The standard curves of both relevant analytes displayed a linear pattern with regression values > 0.999 in the 1–10 μg/mL range. For both herbal markers, 1 μg/mL was the lowest limit of quantification. The method’s accuracy was 100.38-100.93 % and 99.13-100.75 % for with withanolide A, and 12-deoxy-withastramonolide respectively. The precision of within and between days was found in the tolerable limit of >2% for both herbal markers. Conclusion: The suggested method worked well for simultaneously analyzing the extracted samples and identifying withanolides.

Degradation kinetics of betalains in red beetroot juices throughout fermentation process and storage

Contemporary customers have increasingly heightened demands regarding their dietary preferences, favoring readily available and healthful ready-to-consume food and beverage alternatives. In order to fulfill this demand, the beverage industry has been exploring innovative products. Red beetroot juice (RBJ) is easily consumed and offers a beneficial advantage due to its betalain content. Both the traditional/spontaneous method and the industrial method are viable options for producing RBJ. The aim of this study was to examine the stability of betalains, the primary bioactive component in RBJ, throughout the fermentation process and during storage. The RBJ samples contained betalain pigments, as indicated by the infrared spectra. No decrease in betalain content was observed in either RBJ juice fermented by two different methods. The total betalain content of the RBJ samples was 594.068 and 535.152 mg/L at the beginning of fermentation through the spontaneous method and the method with the addition of Lacticaseibacillus paracasei 431 (Lc. paracasei), respectively, and 580.151 mg/L and 667.382 mg/L at the conclusion of fermentation, respectively. Mathematical models were employed to represent the degradation of betalains over time during storage. It was found that the sigmoidal model (R2 = 0.974) and other models (R2 = 0.957–0.969) demonstrated a greater potential to describe the degradation of betalains in RBJ samples produced by the spontaneous method compared to the first-order kinetics model (R2 = 0.932). The models used in the study were successful, with R2 values ranging between 0.927 and 0.932 in the RBJ samples produced with the addition of the probiotic Lc. paracasei for predicting betalain degradation.

Extraction, separation and efficacy of yam polysaccharide

Yam is used as common herbal remedy in traditional Chinese medicine and is grown all over Asia. According to previous research, one of the primary bioactive components of yam is yam polysaccharide. To shed light on the mechanism of yam polysaccharide in ulcerative colitis (UC), a yam heteropolysaccharide named CYP-3a was isolated and purified using ultrasonic extraction, the trichloroacetic acid technique, DEAE cellulose-52 and a Sephadex G75 column. CYP-3a comprises rhamnus: arabinose:galactose:mannose:galacturonic acid glucuronic acid, with a molar ratio of 2.25:4.17:3.30:0.09:0.13:0.26. CCK-8 and ELISA analysis results showed that CYP-3a increased the number of dextran sodium sulphate (DSS)-induced Caco-2 cells and could reduce and inhibit their inflammatory response by lowering the amounts of secreted TNF-α and IL-6. Western blot data demonstrated that CYP-3a at various doses could suppress the endoplasmic reticulum stress–mediated apoptotic pathway generated by DSS-induced UC and down-regulate the protein levels of GRP78, CHOP and NF-κB.

Dihydroavenanthramide D Enhances Skin Barrier Function through Upregulation of Epidermal Tight Junction Expression.

Skin barrier dysfunction and thin epidermis are hallmarks of sensitive skin and contribute to premature aging. Avenanthramides are the primary bioactive components of colloidal oatmeal, a commonly used treatment to enhance skin barrier function. This study investigated the relationship between skin barrier function and epidermal characteristics and explored the potential of dihydroavenanthramide D (dhAvD), a synthetic avenanthramide, to improve the skin barrier. We observed a significant correlation between impaired skin barrier function and decreased epidermal thickness, suggesting that a weakened barrier contributes to increased sensitivity. Our in vitro results in HaCaT cells demonstrated that dhAvD enhances keratinocyte proliferation, migration, and tight junction protein expression, thereby strengthening the skin barrier. To mimic skin barrier dysfunction, we treated keratinocytes and full-thickness skin equivalents with IL-4 and IL-13, cytokines that are implicated in atopic dermatitis, and confirmed the downregulation of tight junction and differentiation markers. Furthermore, dhAvD treatment restored the barrier function and normalized the expression of key epidermal components, such as tight junction proteins and natural moisturizing factors, in keratinocytes treated with inflammatory cytokines. In the reconstructed human skin model, dhAvD promoted both epidermal and dermal restoration. These findings suggest that dhAvD has the potential to alleviate skin sensitivity and improve skin barrier function.

D-glucaro-1,4-lactone improves Diethylnitrosamine induced hepatocellular carcinoma in rats via the uric acid-ROS pathway

Ethnopharmacological relevanceLiuwei dihuang pills is a famous Traditional Chinese Medicine with various anti-cancer properties. Over 50 pharmaceutical manufacturers produce Liuwei dihuang pills in China and an estimated millions of people around the world orally take it every day. D-glucaro-1,4-lactone (1,4-GL) was quantified to be about 12.0 mg/g in Liuwei dihuang pills and a primary bioactive component of it inhibiting the activity of β-glucuronidase in vivo. 1,4-GL can prevent and effectively inhibit various types of cancer. However, its exact mechanism of action remains unknown. The study would justify the traditional usage of Liuwei dihuang pills against cancers. Aim of the study1,4-GL, a bioactive ingredient derived from Liuwei dihuang pills, a famous Traditional Chinese Medicine, could delay the progression of diethylnitrosamine (DEN)-induced hepatocellular carcinoma (HCC) in rats. The mechanism underpinning the effect, however, remains poorly understood. Materials and methodsHealthy and HCC rats were treated with or without 1,4-GL (40.0 mg/kg) and 1HNMR-based metabonomic analysis was employed. 10 metabolites in uric acid pathway were quantitatively determined by UPLC-MS/MS. The expression of xanthine dehydrogenase (XDH), SLC2A9 mRNA, and SLC2A9 protein was determined using RT-qPCR and Western Blot. The effect of 1,4-GL on HCC-LM3 cells was verified in vitro. The alterations of ROS activity, SLC2A9 and XDH gene levels were observed in NCTC-1469 cells induced by lipopolysaccharide (LPS) after 1,4-GL treatment. ResultsAfter the intervention of 1,4-GL, improved pathological morphology, liver lesions in HCC rats was observed with restored serum levels of AFP, AST, ALP, γ-GGT and Fisher's ratio. Hepatic metabonomics revealed that puring metabolism were significantly regulated by 1,4-GL in HCC rats. Uric acid, xanthine and hypoxanthine levels were quantified by UPLC-MS/MS and found to be nearly restored to control levels after 1,4-GL treatment in HCC rats. Changes in xanthine oxidase activity, XDH mRNA expression, and SLC2A9 mRNA and protein expression were also reversed. 1,4-GL treatment in LM3 HCC cells were consistent with the results in vivo. Furthermore, oxidative stress indicators such as T-SOD, GSH, CAT and MDA in serum and liver were improved after HCC rats treated with 1,4-GL. In vitro, 1,4-GL was observed to reduce lipopolysaccharide-induced ROS levels in NCTC-1469 cells with enhanced mRNA and protein expression of SLC2A9 and decreased mRNA level of XDH. ConclusionThe protective effects of 1,4-GL against DEN-induced HCC by reducing uric acid and ROS levels due to down-regulation of uric acid production and up-regulation of SLC2A9 expressions. 1,4-GL may represent a novel treatment that improves recovery from HCC by targeting uric acid-ROS pathway.

Wogonin mitigates acetaminophen-induced liver injury in mice through inhibition of the PI3K/AKT signaling pathway

Ethnopharmacological relevanceScutellaria baicalensis Georgi (SBG), a widely used traditional Chinese medicine, exhibits anti-inflammatory and antioxidant properties. Wogonin is one of the primary bioactive components of SBG. Acetaminophen (APAP)-induced liver injury (AILI) represents a prevalent form of drug-induced liver damage and is primarily driven by inflammatory responses and oxidative stress. Aim of studyTo investigate the therapeutic effects of Wogonin on AILI and the underlying mechanisms. Materials and methodsC57BL/6 J mice were pre-treated with Wogonin (1, 2.5, and 5 mg/kg bodyweight) for 3 days, followed by treatment with APAP (300 mg/kg bodyweight). The serum and liver tissue samples were collected at 24 h post-APAP treatment. Bone marrow-derived macrophages and RAW264.7 cells were cultured and pre-treated with Wogonin (5, 10, and 20 μM) for 30 min, followed by stimulation with lipopolysaccharide (LPS; 100 ng/mL) for 3 h. To examine the role of the PI3K/AKT signaling pathway in the therapeutic effect of Wogonin on AILI, mice and cells were treated with LY294002 (a PI3K inhibitor) and MK2206 (an AKT inhibitor). ResultsWogonin pre-treatment dose-dependently alleviated AILI in mice. Additionally, Wogonin suppressed oxidative stress and inflammatory responses. Liver transcriptome analysis indicated that Wogonin primarily regulates immune function and cytokines in AILI. Wogonin suppressed inflammatory responses of macrophages by inhibiting the PI3K/AKT signaling pathway. Consistently, Wogonin exerted therapeutic effects on AILI in mice through the PI3K/AKT signaling pathway. ConclusionsWogonin alleviated AILI and APAP-induced hepatotoxicity in mice through the PI3K/AKT signaling pathway.

Ganoderic acid A ameliorates depressive-like behaviors in CSDS mice: Insights from proteomic profiling and molecular mechanisms

ObjectiveGanoderic Acid A (GAA), a primary bioactive component in Ganoderma, has demonstrated ameliorative effects on depressive-like behaviors in a Chronic Social Defeat Stress (CSDS) mouse model. This study aims to elucidate the underlying molecular mechanisms through proteomic analysis. MethodsC57BL/6 J mice were allocated into control (CON), chronic social defeat stress (CSDS), GAA, and imipramine (IMI) groups. Post-depression induction via CSDS, the GAA and IMI groups received respective treatments of GAA (2.5 mg/kg) and imipramine (10 mg/kg) for five days. Behavioral assessments utilized standardized tests. Proteins from the prefrontal cortex were analyzed using LC-MS, with further examination via bioinformatics and PRM for differential expression. Western blot analysis confirmed protein expression levels. ResultsChronic social defeat stress (CSDS) induced depressive-like behaviors in mice, which were significantly alleviated by GAA treatment, comparably to imipramine (IMI). Proteomic analysis identified distinct proteins in control (305), GAA-treated (949), and IMI-treated (289) groups. Enrichment in mitochondrial and synaptic proteins was evident from GO and PPI analyses. PRM analysis revealed significant expression changes in proteins crucial for mitochondrial and synaptic functions (namely, Naa30, Bnip1, Tubgcp4, Atxn3, Carmil1, Nup37, Apoh, Mrpl42, Tprkb, Acbd5, Dcx, Erbb4, Ppp1r2, Fam3c, Rnf112, and Cep41). Western blot validation in the prefrontal cortex showed increased levels of Mrpl42, Dcx, Fam3c, Ppp1r2, Rnf112, and Naa30 following GAA treatment. ConclusionGAA exhibits potential antidepressant properties, with its action potentially tied to the modulation of synaptic functions and mitochondrial activities.

Identifying Anti-NSCLC Bioactive Compounds in Scutellaria via 2D NMR-Based Metabolomic Analysis of Pharmacologically Classified Crude Extracts.

We presented a strategy utilizing 2D NMR-based metabolomic analysis of crude extracts, categorized by different pharmacological activities, to rapidly identify the primary bioactive components of TCM. It was applied to identify the potential bioactive components from Scutellaria crude extracts that exhibit anti-non-small cell lung cancer (anti-NSCLC) activity. Four Scutellaria species were chosen as the study subjects because of their close phylogenetic relationship, but their crude extracts exhibit significantly different anti-NSCLC activity. Cell proliferation assay was used to assess the anti-NSCLC activity of four species of Scutellaria. 1H-13C HSQC spectra were acquired for the chemical profiling of these crude extracts. Based on the pharmacological classification (PCA, OPLS-DA and univariate hypothesis test) were performed to identify the bioactive constituents in Scutellaria associated with the anti-NSCLC activity. As a result, three compounds, baicalein, wogonin and scutellarin were identified as bioactive compounds. The anti-NSCLC activity of the three potential active compounds were further confirmed via cell proliferation assay. The mechanism of the anti-NSCLC activity by these active constituents was further explored via flow cytometry and western blot analyses. This study demonstrated 2D NMR-based metabolomic analysis of pharmacologically classified crude extracts to be an efficient approach to the identification of active components of herbal medicine.

Lysimachia capillipes Hemsl. saponins ameliorate colorectal cancer in mice via regulating gut microbiota and restoring metabolic profiles

Lysimachia capillipes Hemsl., a traditional Chinese medicine (TCM), is commonly prescribed for its anti-inflammatory and anti-tumor properties. Pharmacological studies have demonstrated that Lysimachia capillipes Hemsl. saponins (LCS) are the primary bioactive component. However, its mechanism for treating colorectal cancer (CRC) is still unknown. Increasing evidence suggests a close relationship between CRC, intestinal flora, and host metabolism. Thus, this study aims to investigate the mechanism of LCS amelioration of CRC from the perspective of the gut microbiome and metabolome. As a result, seven gut microbiotas and fourteen plasma metabolites were significantly altered between the control and model groups. Among them, one gut microbiota genera (Monoglobus) and six metabolites (Ureidopropionic acid, Cytosine, L-Proline, 3-hydroxyanthranilic acid, Cyclic AMP and Suberic acid) showed the most pronounced callback trend after LCS administration. Subsequently, the correlation analysis revealed significant associations between 68 pairs of associated metabolites and gut microbes, with 13 pairs of strongly associated metabolites regulated by the LCS. Taken together, these findings indicate that the amelioration of CRC by LCS is connected to the regulation of intestinal flora and the recasting of metabolic abnormalities. These insights highlight the potential of LCS as a candidate drug for the treatment of CRC.

Epigallocatechin gallate, the primary bioactive component from Camellia sinensis: A review on immunomodulatory effects in autoimmune diseases by balancing the differentiation of Th and Treg cells

Autoimmune disease is a chronic condition that requires treatment with prolonged use of drugs. Consequently, there is a significant occurrence of adverse effects and toxicity associated with the medicine. On the other hand, epigallocatechin gallate (EGCG), the primary bioactive catechin in green tea (Camellia sinensis), has been demonstrated to possess anti-inflammatory properties and exhibit therapeutic effects in autoimmune disorders. Therefore, EGCG can be considered a complementary and alternative medicine to address the limitations of current treatment. Turning to the disease pathology, the balance between helper T-cell (Th) and regulatory T-cell (Treg) differentiation is the crucial aspect that needs to be regulated in order to attain immunological tolerance and suppress the incidence and severity of autoimmune disease. Here, we aim to comprehensively review the immunomodulatory effect of EGCG on the balance of Th/Treg cell differentiation in diverse autoimmune disorders. Scientific databases, including Scopus, PubMed, Science Direct, and Google Scholar, were searched using the keywords autoimmune AND (epigallocatechin-3-gallate OR epigallocatechin gallate OR EGCG) AND (Thelper OR Th OR Treg OR CD4). Our review revealed that EGCG has ability to repair the imbalance of Th/Treg cell differentiation in rheumatoid arthritis (RA), multiple sclerosis (MS), ulcerative colitis (UC), and autoimmune uveitis (AU) by inhibiting the differentiation of Th1 and Th17 cells while promoting the differentiation of Th2 and Treg cells, as well as improving the clinical conditions of the tested animals. Hence, it might be inferred that EGCG exhibits considerable promise as a viable complementary and alternative therapeutic option for autoimmune disease.

Protective effects of Jing-Si-herbal-tea in inflammatory cytokines-induced cell injury on normal human lung fibroblast via multiomic platform analysis.

The protective effects and related mechanisms of Jing-Si herbal tea (JSHT) were investigated in cellular damage mediated by pro-inflammatory cytokines, including interleukin (IL)-1β, IL-6, and tumor necrosis factor-α, on normal human lung fibroblast by multiomic platform analysis. The in silico high-throughput target was analyzed using pharmacophore models by BIOVIA Discovery Studio 2022 with ingenuity pathway analysis software. To assess cell viability, the study utilized the MTT assay technique. In addition, the IncuCyte S3 ZOOM System was implemented for the continuous monitoring of cell confluence of JSHT-treated cytokine-injured HEL 299 cells. Cytokine concentrations were determined using a Quantibody Human Inflammation Array. Gene expression and signaling pathways were determined using next-generation sequencing. In silico high-throughput target analysis of JSHT revealed ingenuity in canonical pathways and their networks. Glucocorticoid receptor signaling is a potential signaling of JSHT. The results revealed protective effects against the inflammatory cytokines on JSHT-treated HEL 299 cells. Transcriptome and network analyses revealed that induction of helper T lymphocytes, TNFSF12, NFKB1-mediated relaxin signaling, and G-protein coupled receptor signaling play important roles in immune regulatory on JSHT-treated cytokine-injured HEL 299 cells. The findings from our research indicate that JSHT holds promise as a therapeutic agent, potentially offering advantageous outcomes in treating virus infections through various mechanisms. Furthermore, the primary bioactive components in JSHT justify extended research in antiviral drug development, especially in the context of addressing coronavirus.

Patchouli Alcohol: A Potent Tyrosinase Inhibitor Derived from Patchouli Essential Oil with Potential in the Development of a Skin-Lightening Agent

The inhibitory effects of Pogostemon cablin essential oil (patchouli essential oil, PEO) and its primary bioactive compound, patchouli alcohol (PA), on tyrosinase and melanin were investigated in vitro and ex vivo. Treatment with PEO and PA significantly, as well as dose-dependently, reduced forskolin (FRK)-induced melanin biosynthesis, cellular tyrosinase activity, and tyrosinase (TYR) protein expression. However, the transcriptional levels of TYR and tyrosinase-related proteins (TRP-1 and TRP-2) remained unaffected. These results suggest that PEO and PA may directly interrupt tyrosinase enzyme activity, leading to a reduction in melanin biosynthesis. Further experiments supported this notion, revealing that both PEO and PA significantly and dose-dependently inhibited mushroom tyrosinase activity in both the monophenolase and diphenolase phases. Additionally, an in silico molecular docking analysis was performed, utilizing a homology model of human tyrosinase. In conclusion, these findings strongly suggest that patchouli essential oil and its primary bioactive component, patchouli alcohol, hold promise as potential treatments for hyperpigmentary skin conditions and in the development of cosmetic products designed to lighten the skin.

Rapid Determination of Diverse Ganoderic Acids in Ganoderma Using UPLC–MS/MS

Background:: Ganoderma is known for its pharmaceutical, nutritional, and functional benefits. Its primary bioactive components are ganoderic acids. However, previous quantification methods only analyzed an individual or limited number of ganoderic acids. This study aims to develop a reliable method for simultaneously quantifying the major ganoderic acids to enhance Ganoderma quality control and study its active ingredients. Methods:: We developed a rapid quality assessment method to simultaneously determine the eleven ganoderic acids in Ganoderma using ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The sample extraction method, along with mass spectrometric detection and chromatographic separation conditions was optimized. The separation was carried out using the ACQUITY UPLC BEH C18 column with a gradient elution of 0.1% (v/v) formic acid in water and acetonitrile. The mass spectrometry utilized negative mode electrospray ionization (ESI), with quantitative analysis being carried out in the MRM mode. Results:: The calibration curves showed good correlation coefficients (r2 > 0.998). The recovery range was 89.1–114.0%. The intra-day and inter-day relative standard deviation (RSD) were below 6.8% (n = 6) and 8.1% (n = 6), respectively. Furthermore, the detection and quantification limits were 0.66–6.55 μg/kg and 2.20–21.84 μg/kg, respectively. All 11 ganoderic acids in the sample solution remained stable at room temperature for 72 hours. A total of 11 ganoderic acids were quantified in the 13 Ganoderma samples. The levels of ganoderic acids were higher in Ganoderma lucidum than in Ganoderma sinense. Conclusion:: The method developed in this study can quantify ganoderic acids in Ganoderma lucidum, thus establishing a technical foundation for evaluating the Ganoderma quality.

Beneficial endophytic fungi improve the yield and quality of Salvia miltiorrhiza by performing different ecological functions.

Endophytic fungi can enhance the growth and synthesis of secondary metabolites in medicinal plants. Salvia miltiorrhiza Bunge is frequently employed for treating cardiovascular and cerebrovascular ailments, with the primary bioactive components being salvianolic acid and tanshinone. However, their levels in cultivated S. miltiorrhiza are inferior to that of the wild herbs, so the production of high-quality medicinal herbs is sharply declining. Consequently, the utilization of beneficial endophytic fungi to improve the yield and quality of S. miltiorrhiza holds great significance for the cultivation of medicinal plants. In this study, nine non-pathogenic, endophytic fungal strains were introduced into sterile S. miltiorrhiza seedlings and cultivated both in vitro and in situ (the greenhouse). The effects of these strains on the growth indices, C and N metabolism, antioxidant activity, photosynthesis, and content of bioactive ingredients in S. miltiorrhiza were then evaluated. The results showed that the different genera, species, or strains of endophytic fungi regulated the growth and metabolism of S. miltiorrhiza in unique ways. These endophytic fungi primarily exerted their growth-promoting effects by increasing the net photosynthetic rate, intercellular CO2 concentration, and the activities of sucrose synthase, sucrose phosphate synthase, nitrate reductase, and glutamine synthetase. They also enhanced the adaptability and resistance to environmental stresses by improving the synthesis of osmoregulatory compounds and the activity of antioxidant enzymes. However, their regulatory effects on the growth and development of S. miltiorrhiza were affected by environmental changes. Moreover, the strains that significantly promoted the synthesis and accumulation of phenolic acids inhibited the accumulation of tanshinones components, and vice versa. The endophytic fungal strains Penicillium meloforme DS8, Berkeleyomyces basicola DS10, and Acremonium sclerotigenum DS12 enhanced the bioaccumulation of tanshinones. Fusarium solani DS16 elevated the rosmarinic acid content and yields in S. miltiorrhiza. The strain Penicillium javanicum DS5 improved the contents of dihydrotanshinone, salvianolic acid B, and rosmarinic acid. The strains P. meloforme DS8 and B. basicola DS10 improved resistance. Various endophytic fungi affected the quality and yield of S. miltiorrhiza by regulating different physiological and metabolic pathways. This study also provides a novel and effective method to maximize the effects of beneficial endophytic fungi by selecting specific strains to design microbial communities based on the different ecological functions of endophytic fungi under varying environments and for specific production goals.